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Assay Detail

CHEMBL4263045

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of human IKKalpha using ERLLDDRHDSGLDSMKDEE as substrate after 60 mins in presence of ATP by ADP-Glo kinase assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

4-Hydroxy-<i>N</i>-[3,5-bis(trifluoromethyl)phenyl]-1,2,5-thiadiazole-3-carboxamide: a novel inhibitor of the canonical NF-κB cascade.
Pippione AC, Federico A, Ducime A, Sainas S, Boschi D, Barge A, Lupino E, Piccinini M, Kubbutat M, Contreras JM, Morice C, Al-Karadaghi S, Lolli ML.
Medchemcomm (2017) 8 : 1850 -1855
PubMed 30108896 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 4.45 4.45

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4166474 1 4.45
CHEMBL536151 IMD-0354 1.0 1 -
CHEMBL79004 1 -
CHEMBL4287256 1 -
CHEMBL4177097 1 -
CHEMBL4279494 1 -
CHEMBL4284710 1 -
CHEMBL4294749 1 -
CHEMBL4283501 1 -
CHEMBL4280067 1 -
CHEMBL4293673 1 -
CHEMBL4283080 1 -
CHEMBL4290266 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4166474 IC50 = 35500.0 nM 4.45
CHEMBL536151 IMD-0354 IC50 > 100000.0 nM -
CHEMBL79004 IC50 > 100000.0 nM -
CHEMBL4287256 IC50 > 100000.0 nM -
CHEMBL4177097 IC50 > 100000.0 nM -
CHEMBL4279494 IC50 > 100000.0 nM -
CHEMBL4284710 IC50 > 100000.0 nM -
CHEMBL4294749 IC50 > 100000.0 nM -
CHEMBL4283501 IC50 > 100000.0 nM -
CHEMBL4280067 IC50 > 100000.0 nM -
CHEMBL4293673 IC50 > 100000.0 nM -
CHEMBL4283080 IC50 > 100000.0 nM -
CHEMBL4290266 IC50 > 100000.0 nM -